PNU 120596

Pricing Availability Delivery Time Qty
Cat.No. 2498 - PNU 120596 | C13H14ClN3O4 | CAS No. 501925-31-1
Description: Positive allosteric modulator of α7 nAChR; active in vivo
Chemical Name: N-(5-Chloro-2,4-dimethoxyphenyl)-N'-(5-methyl-3-isoxazolyl)-urea
Purity: ≥99% (HPLC)
Datasheet
Citations (8)
Literature

Biological Activity

Positive allosteric modulator of α7 neuronal nicotinic acetylcholine receptors (EC50 = 216 nM), with no detectable effect on α4β2, α3β4 and α9α10 receptors. Active in vivo following systemic administration. Neuroprotective in an in vivo model of transient focal cerebral ischemia.

Compound Libraries

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Technical Data

M. Wt 311.72
Formula C13H14ClN3O4
Storage Desiccate at +4°C
Purity ≥99% (HPLC)
CAS Number 501925-31-1
PubChem ID 311434
InChI Key CEIIEALEIHQDBX-UHFFFAOYSA-N
Smiles COC1=CC(OC)=C(Cl)C=C1NC(=O)NC1=NOC(C)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 31.17 100

Preparing Stock Solutions

The following data is based on the product molecular weight 311.72. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.21 mL 16.04 mL 32.08 mL
5 mM 0.64 mL 3.21 mL 6.42 mL
10 mM 0.32 mL 1.6 mL 3.21 mL
50 mM 0.06 mL 0.32 mL 0.64 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

Hurst et al (2005) A novel positive allosteric modulator of the α7 neuronal nicotinic acetylcholine receptor: in vitro and in vivo characterization. J.Neurosci. 25 4396 PMID: 15858066

Timmermann et al (2007) An allosteric modulator of the α7 nicotinic acetylcholine receptor possessing cognition-enhancing properties in vivo. J.Pharmacol.Exp.Ther. 323 294 PMID: 17625074

Kalappa et al (2013) A positive allosteric modulator of α7 nAChRs augments neuroprotective effects of endogenous nicotinic agonists in cerebral ischemia. Br.J.Pharmacol. [Epub ahead of print] PMID: 23713819


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Keywords: PNU 120596, supplier, Positive, allosteric, modulators, α7, alpha7, a7, nAChR, active, vivo, Nicotinic, Receptors, Acetylcholine, PNU120596, Nicotinic, (a7), Receptors, Tocris Bioscience

8 Citations for PNU 120596

Citations are publications that use Tocris products. Selected citations for PNU 120596 include:

Yamauchi et al (2012) Synthesis of selective agonists for the α7 nicotinic acetylcholine receptor with in situ click-chemistry on acetylcholine-binding protein templates. Nat Commun 82 687 PMID: 22784805

Kasheverov et al (2015) 6-bromohypaphorine from marine nudibranch mollusk Hermissenda crassicornis is an agonist of human α7 nicotinic acetylcholine receptor. Mar Drugs 13 1255 PMID: 25775422

Thomsen et al (2015) α7 and β2 Nicotinic Acetylcholine Receptor Subunits Form Heteromeric Receptor Complexes that Are Expressed in the Human Cortex and Display Distinct Pharmacological Properties. PLoS One 10 e0130572 PMID: 26086615

John et al (2015) Functional α7 nicotinic receptors are expressed on immature granule cells of the postnatal dentate gyrus. PLoS One 1601 15 PMID: 25553616

Chatzidaki et al (2015) Pharmacological Characterisation of Nicotinic Acetylcholine Receptors Expressed in Human iPSC-Derived Neurons. PLoS One 10 e0125116 PMID: 25906356

Zhang et al (2015) Functional Impact of 14 Single Nucleotide Polymorphisms Causing Missense Mutations of Human α7 Nicotinic Receptor. Mol Pharmacol 10 e0137588 PMID: 26340537

daCosta et al (2015) Stoichiometry for α-bungarotoxin block of α7 acetylcholine receptors. J Neurosci 6 8057 PMID: 26282895

Maldifassi et al (2014) A new IRAK-M-mediated mechanism implicated in the anti-inflammatory effect of nicotine via α7 nicotinic receptors in human macrophages. PLoS One 9 e108397 PMID: 25259522


Do you know of a great paper that uses PNU 120596 from Tocris? If so please let us know.

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